Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang Road, Nanjing 210009, China; Zhenjiang Institute for Drug Control, 62 Nanxu Road, Zhenjiang 212000, China.
Department of Natural Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang Road, Nanjing 210009, China.
Bioorg Med Chem Lett. 2014 May 1;24(9):2202-5. doi: 10.1016/j.bmcl.2014.03.004. Epub 2014 Mar 12.
Fifteen novel hybrids containing diterpene skeleton and nitric oxide (NO) donor were prepared from isosteviol. All the compounds were tested on preliminary cytotoxicity, and the results showed that six target compounds (8c, 10b, 14a, 14c, 18c, and 18d) exhibited anti-proliferation activity on HepG2 cells, with 8c (IC50=4.24 μM) and 18d (IC50=2.75 μM) superior to the positive control CDDO-Me (2-cyano-3,12-dioxooleana-1,9(11)-dien-28-acid methyl ester, IC50=4.99 μM); eleven target compounds (8a-c, 9a-c, 10a-b, 14a, 14c, 18d) exhibited anti-proliferation activities on B16F10 cells at different levels, among them, seven compounds were more potent than comptothecin (IC50=2.78 μM) and CDDO-Me (IC50=5.85 μM), particularly, 10b (IC50=0.02 μM) presented the strongest effect, which was selected as a candidate for further study.
从异甜菊醇中制备了 15 种新型含有二萜骨架和一氧化氮 (NO) 供体的杂种。所有化合物均进行了初步细胞毒性测试，结果表明，6 种目标化合物（8c、10b、14a、14c、18c 和 18d）对 HepG2 细胞表现出增殖抑制活性，其中 8c（IC50=4.24 μM）和 18d（IC50=2.75 μM）优于阳性对照 CDDO-Me（2-氰基-3,12-二氧代齐墩果烷-1,9(11)-二烯-28-酸甲酯，IC50=4.99 μM）；11 种目标化合物（8a-c、9a-c、10a-b、14a、14c、18d）在不同水平上对 B16F10 细胞表现出增殖抑制活性，其中 7 种化合物比康普托辛（IC50=2.78 μM）和 CDDO-Me（IC50=5.85 μM）更有效，特别是 10b（IC50=0.02 μM）表现出最强的作用，被选为进一步研究的候选物。
